COMPOUNDING FOR SCALP DISORDERS AND CONDITIONS
Y. Pramar, Ph.D., Professor of Pharmaceutics Xavier University of Louisiana, College of Pharmacy, New Orleans, Louisiana.
Goals: The goals of this article are to provide information on the physiology and disorders of the scalp, and typical drug therapy used to treat these disorders.
Objectives: At the conclusion of this lesson, the reader should be able to: 1. Discuss the physiology of the scalp and the function of the sebum, sweat glands and pores. 2. List at least five disorders/conditions of the scalp. 3. Describe different treatment approaches used in scalp disorders. 4. Become familiar with various formulations used in the treatment of seborrheic dermatitis, dandruff, psoriasis, hair loss, lice and ringworm.
Introduction Scalp disorders may be painful, annoying, unsightly and Pores: The pores in the skin are where the hair follicles embarrassing. Scalp problems may require short-term reside. The pore size is related to sebaceous gland size. treatment, but many of them need long-term therapy Pores enlarge to accommodate a greater oil flow. Acne over months, and sometimes years. Compounding caused by blocked pores often clears up when the pores pharmacists have a significant role in achieving enlarge allowing unimpeded movement of sebum successful therapeutic outcomes in this emerging field. through the pore.
Anatomy and Physiology Sweat Glands: Sweat glands consist of a single tube, the The scalp consists primarily of the skin, sweat glands, lower portion of which is coiled into a ball and the upper sebaceous glands, hair shafts, and hair. When these part (the duct) opens onto the surface of the skin. There appendages are not functioning properly in harmony are two types of sweat glands, the eccrine and the with one another, various scalp disorders can occur. apocrine. The eccrine sweat glands, distributed all over the body, primarily regulate body temperature and Scalp: The scalp is the portion of the body consisting of eliminate toxic substances and waste products; the skin and subcutaneous tissue normally containing hair perspiration is clear and consists of traces of salt, that covers the neuro-cranium. It is especially rich in carbohydrates, protein and oil. The sweat they produce blood vessels; therefore, profuse bleeding may occur is primarily odorless. The apocrine sweat glands are with scalp injuries. The functions of the scalp (skin) primarily in the underarm area, around the nipples and in include protection and excretion. It secretes metabolic the genital area. They are stimulated by the same waste materials and toxins in order to rid the body of hormones that stimulate hair growth in the underarms them. It also secretes sweat to cool the body, and sebum and genital area. The fluid they secrete is milky and rich to protect the skin. in organic material that is subject to bacterial decay, causing body odor. The hair entraps both sweat and Skin: Each layer of the skin (epidermis, dermis, bacteria. subcutaneous) has a specific function. Included in the skin are the sebaceous glands that produce sebum and Sebum: When the sebum gets stuck in the pores, secrete it through the sebaceous ducts into hair follicles, whiteheads, blackheads, papules, pimples and cysts can where it migrates to the surface of the skin. This flow of ultimately occur. It is a result of the sebum getting sebum removes dead skin cells that flake off from inside blocked during its transport and clumping with dead skin the hair follicle. Sebum consists of fatty acids and other cells, being acted upon by bacteria and ultimately substances and protects the skin by reducing the blocking the opening to the skin surface. If pressure evaporation of water from the skin and blocks the builds up, pustules and cysts result. penetration of excess water into the skin. This sebum is one of two constituents making up the lipid film present Hair: Hair grows on the scalp and each hair filament on the skin surface, the other being the lipids of the originates in a deep hair follicle which penetrates into epidermal cells. the dermis. At the base of the follicle is the papilla which is the center of hair growth containing the capillaries and nerves that supply the hair. As new cells Treatment: The treatment selected for psoriasis of the are formed and older cells are pushed upward, they scalp is based on its extent and severity. Therapy can be gradually die and harden into a hair shaft, consisting of initiated using a corticosteroid preparation. Other two layers, the cuticle and cortex. The outer layer, the measures include tar preparations, such as coal tar cuticle, consists of flat, colorless, overlapping cells. The solution (LCD, Liquor Carbonis Detergens), anthralin, cortex contains pigment and a tough protein called calcipotriene and tazarotene. Treatment can be initiated keratin, forming the bulk of the hair shaft. Coarse hair, with a tar shampoo used daily. For thick scales on the as on the scalp, contains an additional inner core called scalp, a 6% salicylic acid gel, or a phenol : mineral oil : the medulla. The hair is lubricated by sebaceous glands glycerin mixture can be used. Alternatively, that are located in the hair follicle. In general, human fluocinolone acetonide 0.01% in oil can be applied under scalp hair is shed every two to four years; body hairs are a shower cap at night followed by tar shampoo in the shed more frequently. morning. Corticosteroids such as triamcinolone, fluocinolone, betamethasone dipropionate, fluocinonide, Hair growth: Hair growth is cyclical, consisting of three amcinonide, or clobetasol in solution form can be used phases. The growing phase is the “Anagen” phase; twice daily. about 90% of scalp hairs are in the anagen phase at any point in time. On a daily basis, about 50 to 100 scalp Hair Loss follicles go into the resting phase, or the “Catagen” I. Description: Pattern, or androgenetic baldness, is the phase, which involves 1% of the hairs daily. The most common form of alopecia. It is of genetic shedding phase is the “Telogen” phase and predetermination with the earliest changes occurring on approximately 10-20% of scalp hairs may be in the the front sides of the scalp and at the crown of the skull. telogen phase at any point in time. The extent of hair loss is variable and unpredictable, but may be experienced by approximately 80% of all men.
SCALP DISORDERS AND THEIR TREATMENT Treatment: A 5% solution of minoxidil alone or in combination with other active ingredients can be used in Seborrheic Dermatitis and Dandruff both male and female patients, generally twice daily. Description: Seborrheic dermatitis is an acute or chronic Those that respond are usually less than five years into papulosquamous dermatitis presenting with dry scales their hair loss. and underlying erythema. In some cases pruritis is present. Dandruff occurs when there is a mild scaling II. Description: Alopecia areata is believed to be the without any erythema, and can occur if the scalp is dry result of an imuunologic process. Typically, there are or oily. It may be the result of several factors, including patches that are smooth, without scarring. Tiny hairs, hormonal imbalance, impaired metabolic nutrition, diet, generally 2-3 mm in length, may be seen. In some cases, tension, increased bacterial and fungal activity, all the scalp hair may eventually be involved. Alopecia biochemical changes in the scalp, the use of topical areata is a self-limiting disease where there may be medications and cosmetics. Seborrheic dermatitis complete re-growth of hair in about 80% of cases. In occurs when there is general erythema without tight, some cases, mild alopecia areata is resistant to therapy. thick, silvery scales. Psoriasis is evidenced by the presence of well-demarcated red plaques. Treatment: Severe forms may be treated by systemic corticosteroids; however, recurrences generally occur Treatment: Routine treatment for seborrhea of the scalp when therapy is discontinued. Corticosteroids can also involves a shampoo that may contain tar, zinc pyrithione be administered intralesionally; for example or selenium, used daily if necessary. A ketoconazole 1% triamcinolone acetonide 2.5 to 10 mg/mL can be injected or 2% shampoo can be used twice weekly. If needed, in aliquots of 0.1 mL every 1 to 2 cm in the involved solutions or lotions of topical corticosteroids can be used areas. The total dose should not exceed 30 mg per twice daily. month for adults. Another treatment includes daily use of anthralin 0.5% ointment. Psoriasis Description: Psoriasis is an inflammatory skin disease Other therapeutic approaches involve the use of topical that may be based upon a genetic predisposition. When diphenylcyclopropenone and squaric acid dibutyl ester. the skin is injured or irritated, it tends to induce lesions These agents serve to sensitize the skin; this is followed of psoriasis at the site. There are several variants of by application of progressively weaker concentrations psoriasis, with the most common being the plaque type. designed to produce a slight dermatitis. This results in Psoriasis presents as silvery scales on bright red, well- hair re-growth in 3 to 6 months in some patients. demarcated plaques that may be accompanied by itching. 2 III. Description: Drug-induced alopecia may result from Rx Hydrocortisone 1% Antipruritic Scalp Lotion thallium, excessive vitamin A, retinoids, antimitotic Hydrocortisone 1 g agents, anticoagulants, antithyroid drugs, oral Menthol 250 mg contraceptives, trimethadione, allopurinol, propranolol, Polysorbate 80 0.25 mL indomethacin, amphetamines, salicylates, gentamicin Ethanol 95% 25 mL and levodopa. Drug-induced alopecia is very Propylene glycol 25 mL disconcerting to the patient, but it is reversible when the Purified water, qs 100 mL causative agent is discontinued. Mix the hydrocortisone and menthol with the Treatment: No real treatment is indicated in such cases, Polysorbate 80. Add the propylene glycol and ethanol other than discontinuation of the causative agent. and mix well. Add sufficient purified water to volume and mix well. Package and label. Lice Description: Pediculus humanus var capitis (the head Formulations for Seborrheic Dermatitis and louse, approximately 3-4 mm long) is the causative Dandruff agent for pediculosis of the skin of the scalp. It is Rx Selenium Sulfide 1% Shampoo presented as pruritis with excoriation and the presence of nits on hair shafts; they are easiest to see above the ears Selenium Sulfide 1 g and at the nape of the neck. Head lice can be spread by Propylene glycol 5 mL individuals sharing hats or combs and it is epidemic Shampoo vehicle (commercial), qs 100 mL among children of all socioeconomic classes, especially Levigate the selenium sulfide with the propylene glycol. in elementary schools. Adults in close contact with Add the shampoo vehicle to volume and mix well. children may also get the infestation. Package and label.
Treatment: Options for treating head lice include Rx Zinc Pyrithione 1% Shampoo. ivermectin 0.8% lotion, malathion 0.5% or 1% lotion, Zinc pyrithione 1 g (equivalent) permethrin 1% cream rinse and pyrethrins 0/17% to Propylene glycol 10 mL. 0.33%. The ivermectin lotion is left on for 8 to 12 hours Shampoo vehicle (Commercial), qs 100 mL prior to rinsing off. The malathion is applied to the scalp and left on for about 12 hours. The permethrin cream Levigate the zinc pyrithione with the propylene glycol. rinse is left on from 30 minutes to 8 hours prior to Add the shampoo vehicle to volume and mix well. rinsing off and treatment is repeated in one week. Package and label. Following application of these preparations, it is Rx Triamcinolone 0.1% Scalp Lotion important to meticulously remove the nits with a fine- tooth comb. Triamcinolone 100 mg Propylene glycol 25 mL Ringworm Ethanol 95% 25 ml Description: Ringworm presents as a ring-shaped lesion Purified Water, qs 100 mL with an advancing scaly border and central cleared area, Mix the triamcinolone with the propylene glycol and or as scaly patches with a distinct border on the skin or ethanol. Add sufficient purified water to volume and scalp. The affected areas may also itch. Trichophyton mix well. Package and label. rubrum is the most common causative agent. Rx Anti-Seborrhea Clear Lotion Treatment: Many of the topical antifungal agents can be used, including miconazole, clotrimazole, ketoconazole, Progesterone 500 mg econazole, sulconazole, oxiconazole, ciclopirox, Ethanol 95% 10 mL butenafine and terbinafine. Topical dosage forms Ethoxy diglycol 50 mL commonly used include creams, solutions and gels. If Methylparaben 50 mg the product is expected to be exposed to a wet Propylparaben 20 mg environment, an ointment would be more appropriate. Propylene glycol 1 mL Treatment should be continued up to two weeks after Purified water, qs 100 mL symptoms have resolved. Dissolve the progesterone in the ethanol. Add the
ethoxy diglycol. Dissolve the methylparaben and FORMULATIONS FOR TREATING SCALP propylparaben in the propylene glycol and add to the DISORDERS AND CONDITIONS progesterone solution. Add sufficient purified water to volume and mix well. Package and label. General Applications for Pruritus of the Scalp 3 Rx Sulfur Shampoo Coal tar 1 g
Sulfur (colloidal) 1 g Polysorbate 80 2 g Aquaphor, qs 100 g Magnesium aluminum silicate 1 g Ammonium lauryl sulfate 40 g Mix the coal tar with the polysorbate 80 and incorporate Lauramide DEA 4.5 g the anthralin. Incorporate into the Aquaphor and mix Sodium chloride 200 mg until uniform. Package and label. Methylparaben 50 mg Rx Anthralin 1% Medication Stick Propylparaben 20 mg Purified water, qs 100 mL Anthralin 200 mg
Slowly add the magnesium aluminum silicate to about Polyethylene glycol 3350 6.5 g Polyethylene glycol 300 15 mL 50 mL of purified water while agitating and mix until smooth and uniform. Add the colloidal sulfur, Mix the polyethylene glycols together by heating to a ammonium lauryl sulfate, lauramide DEA, sodium temperature of about 550C. Incorporate the anthralin and chloride, methylparaben and propylparaben and mix mix well. Pour into medication stick molds and allow to well. Add sufficient purified water to volume and mix cool. Package and label. well. Package and label. Rx Calcipotriene 0.003% Lotion Rx Phenol, Glycerin and Mineral Oil Shake Lotion Calcipotriene 0.005% Cream 60 g Phenol 1 g Propylene glycol, qs 100 mL
Glycerin 10 mL Mix the commercial calcipotriene 0.005% cream with Purified water 20 mL sufficient propylene glycol to make 100 mL. Package Methylparaben 50 mg and label. Propylparaben 20 mg Mineral Oil, Light, qs 100 mL Rx Fluocinolone Acetonide 0.01% in Oil
Dissolve the phenol, methylparaben and propylparaben Fluocinolone acetonide 10 mg in the glycerin. Add the purified water and mix well. Vegetable oil, qs 100 mL
Add the mineral oil and agitate. This is not an emulsion, Incorporate the fluocinolone acetonide into a vegetable but is an immiscible shake-type lotion. oil, such as sesame oil, or almond oil, and mix well.
Formulations for Psoriasis Package and label.
Rx Coal Tar Shampoo Formulations for Hair Loss
Coal tar solution 2.8 g Rx Minoxidil 5% and Retinoic Acid 0.01% Scalp Polysorbate 80 5 mL Lotion Shampoo vehicle (commercial), qs 100 mL Minoxidil 5 g Mix the coal tar solution with the polysorbate 80. Retinoic acid 10 mg Incorporate the shampoo vehicle and mix well. Package Propylene glycol 20 mL and label. Ethanol 95%, qs 100 mL
Rx Coal Tar and Salicylic Acid Scalp Lotion Mix the minoxidil and retinoic acid with the propylene glycol. Add sufficient ethanol to volume and mix well. Coal tar solution 10 mL Package and label. Salicylic acid 6 g Polysorbate 80 1 mL Rx Minoxidil 2% and Finasteride 0.1% Scalp Lotion Ethanol 95% 20 mL Propylene glycol, qs 100 mL Minoxidil 2 g Finasteride 100 mg Mix the polysorbate 80 with the coal tar solution. Mix Propylene glycol 20 mL the salicylic acid with the alcohol and about 60 mL of Ethanol 95%, qs 100 mL the propylene glycol. Add the coal tar solution mixture slowly with mixing to the propylene glycol mixture. Pulverize the required number of finasteride tablets and Add sufficient propylene glycol to volume and mix well. mix with about 75 mL of ethanol in a covered container Package and label. and let sit for a couple of hours. Filter through a paper filter to remove the excipients. Add the minoxidil and Rx Anthralin 1% and Coal Tar 1% Ointment propylene glycol to the filtrate and mix well. Add
Anthralin 1 g 4 sufficient ethanol to volume and mix well. Package and mortar with a pestle to ensure uniform and small particle label. size of the ivermectin. Package and label.
Rx Spironolactone Scalp Lotion Rx Ivermectin 1% Lotion
Spironolactone 1 g Ivermectin 1 g Methylcellulose 0.25 g Propylene glycol 15 mL Ethanol 95% 40 mL Dermabase 30 g Propylene glycol 20 mL Purified water, qs 100 mL
Purified water, qs 100 mL Mix the ivermectin with the propylene glycol to form a
Mix the spironolactone and methylcellulose with the smooth paste using a mortar and pestle. Incorporate the propylene glycol. Add the ethanol and mix well. Add Dermabase and mix well. Slowly add sufficient purified sufficient purified water to volume and mix well. water to volume and mix well. Package and label. Package and label. Formulations for Ringworm
Rx Diphenylcyclopropenone 0.1% to 2% Solutions Rx Clotrimazole 1% Scalp Lotion
Diphenylcyclopropenone 100 mg to 2 g Clotrimazole 1 g Acetone, qs 100 mL Propylene glycol 50 mL Dissolve the diphenylcyclopropenone in sufficient Polyethylene glycol 300, qs 100 mL acetone to volume. Package and label. Caution: Dissolve the clotrimazole in the propylene glycol and Diphenylcyclopropenone is a strong sensitizing agent. add sufficient polyethylene glycol 300 to volume and Exercise care when preparing these solutions; wear mix well. Package and label. appropriate masks, garb and gloves. Rx Miconazole 1% and Tolnaftate 1% Scalp Lotion Rx Squaric Acid Dibutyl Ester 0.1% to 1% Solutions Miconazole 1 g Squaric acid dibutyl ester 100 mg to 1g Tolnaftate 1 g Acetone or Ethanol 95%, qs 100 mL Propylene glycol 50 mL
Polyethylene glycol 300, qs 100 mL Dissolve the squaric acid dibutyl ester in sufficient acetone OR ethanol to volume. Package and label. Dissolve the miconazole and tolnaftate in the propylene glycol and add sufficient polyethylene glycol 300 to Formulations for Lice Infestation volume and mix well. Package and label.
Rx Malathion 0.5% Topical Lotion Rx Ketoconazole 2% Solution
Malathion 500 mg Ketoconazole 2 g Isopropyl alcohol 70% 70 mL Polyethylene glycol 300 80 mL Lavender oil 30 drops Propylene glycol 20 mL
Bay oil 3 drops Dissolve the ketoconazole in the polyethylene glycol Ethanol 95%, qs 100 mL 300 and propylene glycol and mix well. Package and Note: Compound this preparation in a well-ventilated label. area or use an exhaust hood, since malathion fumes can Note: With the exception of a few formulations be irritating to the mucous membranes of the nasal containing drugs such as triamcinolone, fluocinolone passages. Wear disposable gloves to prevent retention acetonide, spironolactone, finasteride, and squaric acid of odor on the hands. dibutyl ester, the remaining preparations can be Disperse the malathion in the isopropyl alcohol. Add the dispensed over-the-counter. fragrances and mix well. Add sufficient ethanol to volume and mix well. Package and label. References 1. ‘A practical guide to contemporary pharmacy practice’ by Rx Ivermectin 1% Creme Rinse Judith E. Thompson, Third Edition. Lippincott, Williams
Ivermectin 1 g & Wilkins. 2009 2. ‘Pharmaceutical Dosage Forms and Drug Delivery Polyethylene glycol 300 17 mL Systems’ by Howard C. Ansel, Nicholas G. Popovich, and Creme Rinse (Commercial), qs 100 mL Loyd V. Allen, Jr. Ninth Edition. Lippincott, Williams &
Mix the ivermectin with the polyethylene glycol 300 to Wilkins. 2011. 3. ‘The Art, Science, and Technology of Pharmaceutical form a smooth paste. Incorporate the creme rinse and Compounding’ by Loyd V. Allen, Jr. Third Edition. mix well. It may be necessary to work the product in a American Pharmacists Association. 2008.
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